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Method for preparing clarithromycin granule without bitter taste

A technology of clarithromycin and bitterness, which is applied in the field of preparation of clarithromycin drug pellets, can solve the problems of affecting curative effect, decreased compliance with doctor's orders, etc., and achieves the effects of good therapeutic effect, abundant dosage forms and simple preparation method.

Inactive Publication Date: 2009-08-12
上海微丸医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Due to the unbearable bitterness of clarithromycin itself, some oral preparations such as: granules, dispersible tablets, suspensions, etc. patients' compliance with doctor's orders is greatly reduced, until the curative effect is affected

Method used

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  • Method for preparing clarithromycin granule without bitter taste
  • Method for preparing clarithromycin granule without bitter taste
  • Method for preparing clarithromycin granule without bitter taste

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Preparation of clarithromycin debitter granules

[0033] (1) Preparation of coating solution:

[0034] Solution A: Take 100g of glyceryl monostearate, Tween-805g, 1200g of pure water, and stir well;

[0035] Solution B: Take Eudragit L30D55 ​​5880g, triethyl citrate 176g, microcrystalline cellulose 100g, pure water 3700g, stir well.

[0036] Solution C: Take 60g of Eudragit E-100, 1140g of 95% ethanol, fully stir to dissolve,

[0037] Then, add pure water to solution A, solution B and solution C to 18520g, set aside.

[0038] (2) Coating

[0039] Take 2000g 80 mesh clarithromycin, and the coating parameter is fluidized coating drying. 2ml / min. After spraying, continue to dry for 20 minutes, granulate, take pellets with a diameter of 80-800 μm, clarithromycin content: 48.5%, and other items meet the quality standards.

[0040] (2) Preparation of clarithromycin dry suspension

[0041] Specifications: Each bag contains clarithromycin 100mg, 2g / bag, when taking i...

Embodiment 2

[0045] Preparation of clarithromycin debitter granules

[0046] (1) Preparation of coating solution:

[0047] Solution A: Take 300g of glyceryl monostearate, 12g of Sipan 20-100, 500g of pure water, and stir well;

[0048] Solution B: Take 5880g of Eudragit L30D55, 120g of butylene sebacate, 180g of diethyl phthalate, 100g of microcrystalline cellulose, 5100g of pure water, and stir well.

[0049] Solution C: Take 100g of No. II acrylic resin, 1000g of 95% ethanol, fully stir to dissolve,

[0050] Then, add pure water to solution A\solution B and solution C to 19250g, set aside.

[0051] (2) Coating

[0052] Take 2000g 60 mesh clarithromycin, the coating parameters are fluidized coating and drying, first preheat the coating system to 38°C, and spray coating, control the inlet temperature to 45°C, the atomization pressure to 0.32MPa, and the spray liquid flow 60ml / min. After spraying, continue to dry for 20 minutes, granulate, take pellets with a diameter of 80-800 μm, clari...

Embodiment 3

[0054] Preparation of clarithromycin debitter granules

[0055] (1) Preparation of coating solution:

[0056] Solution A: Take polyethylene glycol 200-20000 450g, Tween-8015g, pure water 1800g, stir well;

[0057] Solution B: Take Eudragit L30D55 ​​5880g, butylene sebacate 300g, microcrystalline cellulose 100g, pure water 3500g, stir well.

[0058] Solution C: Take 120g of No. III acrylic resin, 2280g of 95% ethanol, fully stir to dissolve,

[0059] Then, add pure water to solution A\solution B and solution C to 21300g, set aside.

[0060] (2) Coating

[0061] Take 2000g 120 mesh clarithromycin, the coating parameters are fluidized coating and drying, first preheat the coating system to 38°C, and carry out spray coating, control the inlet temperature at 60°C, the atomization pressure at 0.45MPa, and the spray liquid flow rate 120ml / min. After spraying, continue to dry for 20 minutes, granulate, take pellets with a diameter of 80-800 μm, clarithromycin content: 30.5%, and ...

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PUM

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Abstract

The invention relates to a method for preparing clarithromycin debitterized granules, which comprises the following steps: (1) preparing solution of coating: preparing solutions A, B and C respectively, then, mixing the solutions evenly, and adding pure water for later use; and (2) coating: coating 2,000g of 60 to 120-mesh powdery clarithromycin with the coating solution with the specific coating parameters being fluidized coating / drying; preheating the coating system to the temperature of 38 DEG C, and spraying the coating system with the inlet temperature being 36 to 60 DEG C, the atomization pressure being 0.08 to 0.45 MPa and the flow rate of the spray solution being 2 to 120 ml / min; and proceeding with drying for 20min and collecting pellets with the pellet diameter being 80 to 800 Mum. The invention has the advantages that the materials are easily obtainable, the cost is low and the preparation method is simple and environment-friendly, therefore, the method is favorable for industrialized production; moreover, the prepared granules solve the problem that the bitter taste is insufferable during the oral administration and make the forms of the oral preparation richer and the range of those who take the granules wider, and the granules are particularly suitable for children to take.

Description

technical field [0001] The invention belongs to the field of preparation of clarithromycin drug pellets, in particular to a preparation method of clarithromycin debitter granules. Background technique [0002] Clarithromycin, also known as clarithromycin, chemically named 6-O-methylerythromycin, is a derivative of erythromycin and belongs to macrolide antibiotics. Molecular formula: C38H69NO13; molecular weight: 747.96, chemical structural formula: [0003] [0004] Clarithromycin is a white or off-white crystalline powder; it is odorless and has a very bitter taste. Soluble in chloroform, soluble in acetone or ethyl acetate, slightly soluble in methanol or ethanol, insoluble in water. [0005] Clarithromycin was successfully developed by Japan's Taisho Corporation in the early 1990s and registered under the trade name Clarith. Afterwards, Dazheng Company first transferred its technology to Abbott of the United States for production; it was launched in Ireland and Ital...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/7048A61K47/38A61K47/34A61P31/04A61K47/10A61K47/26A61K47/32
Inventor 蒋健庆
Owner 上海微丸医药开发有限公司
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